ES2344002T3 - USE OF CATIONIC SURFACTANT AS A POTENTIATOR OF ANTIMICROBIAL ACTIVITY IN DEODORANTS AND ORAL CARE. - Google Patents

Abstract

The antimicrobial system comprising a cationic surfactant, which the cationic surfactant is the ethyl ester of arginine hydrochloride lauramide (LAE), according to the following formula: ** (See formula) ** and at least one selected antimicrobial agent from the group consisting of 2,4,4-trichloro-2-hydroxy-diphenyl (triclosan), 3,4,4-trichlorocarbanilide (triclocarbano) and 2-phenoxyethanol, the antimicrobial system that is characterized by its increased activity.

Description

Use of cationic surfactant as an enhancer of Antimicrobial activity in deodorants and oral care.

This invention relates to a new use of cationic surfactants as enhancers of the activity of the Traditional antibiotics and preparations according to this new use of deodorants and oral care.

Many antibiotics are known to be effective against specific and general bacteria that are present in the oral cavity and bacteria like the one that are responsible for body odor. However, most of they show incompatibilities with human skin and membranes mucous membranes of the oral cavity, such as irritations and allergies and They are toxic to humans too.

On the other hand, it has been shown that cationic surfactants derived from lauric acid and arginine are biologically active substances, in particular, the ethyl ester of lauramide of arginine monohydrochloride, hereinafter, called LAE. LAE has the chemical structure of formula (1).

one

The preparation of this product has been described. in a number of different patents.

Biological studies conducted in different research centers under the supervision of the applicant of the The present invention showed that LAE acts primarily on the outer and cytoplasmic membrane of microorganisms and also, to the cytoplasmic environment, preventing its proliferation. His action it will depend on the type of microorganism and the time of exposition.

In addition, its metabolism in rats has been studied showing rapid absorption and metabolization in amino acids and natural lauric acid fatty acids, which is finally excreted in the form of carbon dioxide and urea. Toxicological studies have shown that LAE is completely harmless to animals and humans.

We have found that combinations of LAE with Traditional antibiotics have better LAE activity or these antimicrobials by themselves in test applications. This improvement in the activity of LAE MDY is explained by its action on the cytoplasmic membrane of microorganisms.

Thus, it was the object of this invention, provide more antimicrobial systems for products skin cosmetics and oral care, in particular, with the aim to provide systems that comprise small amounts of traditional antimicrobials in view of the risk of Lack of tolerance.

The use of the invention refers to LAE of the previous formula (1).

This antimicrobial system is characterized by Your biggest activity. Now it has been discovered that the activity antimicrobial of LAE combinations with antimicrobials as defined in claim 1 used in the formulations and preparations for skin and oral care is greater than the activity developed by each of the components when use the dose alone. An increase in activity when the amounts of the compounds of formula (1) and of antimicrobials are reduced.

Thus, toxic adverse effects and / or irritation and / or allergy shown by antimicrobial systems have been reduced.

LAE is used in association with antimicrobials common, such as 2,4,4-trichloro-2-hydroxy diphenylether  (triclosan), 3,4,4-trichlorocarbanilide (triclocarbano), and 2-phenoxyethanol, for formulation of cosmetics and preparations aimed at avoiding body odor and to provide oral care, which apply to the epidermis or in the teeth and in the mucous membranes of the oral cavity, in order to clean, perfume and / or change the smell body and / or protect a good physical condition.

The antimicrobial system of the invention comprises the cationic surfactants of formula (1) in a amount of 0.001 to 1% by weight and the concentration of the agent traditional antimicrobial as defined in claim 1 from 0.0001% to 2% by weight with respect to the total weight.

The antimicrobial system of the invention it comprises, in particular, more a preferred amount of traditional antimicrobial agent in deodorant applications, from 0001 to 0.5% by weight of 2,4,4-trichloro-2-hydroxyydiphenylether (triclosan) and / or from 0001 to 1.5% by weight, of 3,4,4-trichlorocarbanilide (triclocarbano) and / or 0.001 to 1% by weight of 2-phenoxyethanol.

And the amount of the antimicrobial agent Traditional in oral care applications is 0001 to 0.3% by weight of 2,4,4-trichloro-2-hydroxydifenyleter (triclosan).

The composition of this invention comprises a medium that is compatible with the skin, mucous membranes, and the hair. These compositions may contain the components Common, such as: fatty compounds such as oils minerals, animal fat oil, vegetable oil, synthesis and silicone, as well as alcohols, fatty acids and waxes, solvents organic, surface active agents, solubilizers and ionic and non-ionic emulsifiers, thickening hydrophilic agents and gelatifiers, such as carboxyvinyl polymers (Carbomer, for example), acrylic copolymers (for example, acrylates and alkylene acrylates), polyacrylamides, polysaccharides; natural gums (for example, xanthan gum), lipophilic agents thickeners and gelatifiers, such as modified clays (e.g., bentonite), salts of metallic fatty acids, silica hydrophobic and polyethylene, perfumes and essential oils; astringent; antiperspirants; fluorides; moisturizers, sweeteners, softeners, excipients, antioxidants, agents sequestrants, opacifiers, filters; coloring compounds that they are lipophilic or hydrophilic, and pigments: ingredients hydrophilic or lipophilic active. These compositions can also contain more antimicrobial agents that are different from those defined in the claims.

The amounts of these usual components mentioned in the previous paragraph are the normal ones used in this field. These components add to the systems to the antimicrobials of the invention, without having any influence on the His composition.

In accordance with the invention the compositions they can be in different cosmetic forms suitable for a topical application, such as:

a) Single phase systems:

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water or solution hydro-glycolic containing one or more agents surfactants that are used for cleaning the skin and mucous membranes;

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Water, hydro-alcoholic, hydro-glycolic or oil solution, which may contain other additives to be used in general care and / or protection for the skin and / or the mucous membranes;

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Water, hydro-alcoholic, hydro-glycolic or oily gel, which may contain other additives to be used  in general care and / or protection for the skin and / or mucous membranes

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solid anhydrous products that may contain other additives to be used in care General and / or protection for skin and / or membranes mucous

b) Biphasic Systems:

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Water, hydro-alcoholic, hydro-glycolic or oily gel, which may contain other additives to be used in care General and / or protection for skin and / or membranes mucous membranes;

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solid anhydrous products that may contain other additives to be used in care General and / or protection of the skin and / or membranes mucous

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emulsions formed by the dispersion of an oil phase in a water phase (O / W) or in a reverse phase (W / O), which will be used in general care and / or the protection of the skin of the face and / or membranes mucous

c) and combinations of the other systems that they form multiphase systems, suspensions and emulsions of microemulsions

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The compositions that have been mentioned previously they can also be used as an aerosol, or as aerosol compositions and may contain a propulsion agent under pressure.

Thus, the compositions of the invention can have the appearance of a cream, a lotion, a milk, an emulsion, a gel or one of a skin oil, a salt, a gel, a foam / spray or a bath and shower oil and in any case Aspects shown.

The compositions according to the invention have been prepared according to the usual well known techniques for An expert in the field.

Procedure to evaluate the effectiveness of the system antimicrobial

Antimicrobial systems have been evaluated by the inhibition zone method (adapted by the Association Analytical Chemistry Officer, J. Assoc. Off. Anal. Chem., 62, 466-467 (1982)), using specific tests of micro-organisms These microorganisms were:

for oral care products of evaluation:

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for deodorant products from evaluation:

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The method is to measure the area of inhibition created by the antimicrobial system of each of the Cosmetic compositions, placed in a medium hole, for each micro-organism test.

Each microorganism test was inoculated in the appropriate culture medium with an objective concentration of 10 6 cfu (colony forming unit) / ml, approximately, and 20 ml of inoculated medium were inoculated pipetted into plates Petri and we let them grow. It is also possible to sow the microorganisms on the surface of the sterile medium if it is suitable.

A 15 mm diameter hole was made in the medium and 0.5 mL of the cosmetic composition was deposited in the the hole. It is allowed to diffuse one hour and then incubated.

The temperature remained at the optimum value for each microorganism and the plates were protected against light.

Each trial was performed in triplicate.

The radius of the zone of inhibition was measured at 24 hours for bacteria and 4 days later for yeasts cosmetic compositions in which it was placed.

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Examples

Different examples of preparation formulas Cosmetics according to the invention have been tested. The examples show only one selection, and do not represent a restriction to use of the antimicrobial system in other cases.

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The concentrations of the antimicrobial agents used in the following examples are shown in the
Table 1:

TABLE 1

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The activity of each antimicrobial system is relates to the activity of the antimicrobial system 1 through Its radius of inhibition. The resulting value is used for compare the activity of traditional antimicrobial agents with and without LAE. Therefore, a higher value of this parameter represents a greater antimicrobial activity in relation to the 0.3% in the LAE system.

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Example mouthwash Example 1

The composition of a direct use of rinse oral, tests the effectiveness of antimicrobial systems, is (in g):

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This formulation is completed with an amount suitable of the antimicrobial system of the invention and its activity antimicrobial is evaluated with the traditional formulations of antimicrobial agents used alone.

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The results are shown in table 2.

TABLE 2

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It is shown in Table 2 that the combination of LAE with traditional antibiotics leads to effects that are higher than those shown by these compounds when used alone, with the advantages described above.

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Examples of dentifrices Example 2

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This formulation is completed with an amount suitable of the antimicrobial system of the invention and its activity antimicrobial is evaluated against traditional formulations of antimicrobial agents used alone.

The results are shown in table 3.

TABLE 3

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It is shown in table 3 that the combination of LAE with common antimicrobials leads to the effects that are equal to or greater than those shown by these compounds when use alone, with the advantages described above.

Other examples of toothpaste preparation, where antimicrobial systems were also analyzed, it describe those in examples 3 to 5. The experimental results obtained in example 2 are representative of these examples.

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Example 3

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Example 4

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Example 5

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Deodorant Examples Example 6

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This formulation is completed with an amount suitable of the antimicrobial system of the invention and its antimicrobial activity is evaluated against formulations Traditional antimicrobial agents used alone.

The results are shown in table 4.

TABLE 4

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It is shown in Table 4 that the activity of a combination of LAE with common antimicrobials is equal or greater  than those shown in these compounds when used alone, with the advantages described above.

Other examples of deodorants, where Antimicrobial systems were also tested, described in The following preparation examples 1 to 5. The results Experimental results obtained in Example 6 are representative for these preparation examples too.

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Preparation Example one

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Preparation Example 2

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Preparation Example 3:

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Preparation Example 4

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Preparation Example 5

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References cited in the description This list of references cited by the applicant Its sole purpose is the convenience of the reader. It is not part of European Patent document. Although great care has been taken in the compilation of references, errors cannot be excluded or omissions and the EPO rejects any responsibility in this sense. Non-patent related literature cited in the description

J. Assoc. Off. Anal. Chem ., 1982 , vol. 62, 466-467.

Claims (11)

1. The antimicrobial system comprising a cationic surfactant, which the cationic surfactant is the ester ethyl arginine hydrochloride lauramide (LAE), according with the following formula: 19 and at least one antimicrobial agent selected from the group consisting of 2,4,4-trichloro-2-hydroxy-diphenyl (triclosan), 3,4,4-trichlorocarbanilide (triclocarbano) and 2-phenoxyethanol, the antimicrobial system characterized by Your biggest activity. 2. The antimicrobial system, according to the claim 1 wherein the concentration of cationic surfactant It is 0.001 to 1% by weight and concentration of agent antimicrobial from 0.0001% to 2% by weight in relation to the total weight of the antimicrobial system. 3. The antimicrobial system according to the claim 2, wherein the amount of the antimicrobial agent in Deodorant applications is 0001 to 0.5% by weight, of 2,4,4-trichloro-hydroxy-diphenyl (triclosan) and / or from 0001 to 1.5% by weight, of 3,4,4-trichlorocarbanilide (triclocarbano) and / or from 0001 to 1% by weight, of 2-phenoxyethanol. 4. The antimicrobial system according to the claim 2, wherein the amount of the antimicrobial agent in the  Oral care applications is 0001 to 0.3% by weight, of 2,4,4-trichloro-hydroxy-diphenyl (triclosan). 5. Antimicrobial system according to any one of claims 1 to 4, further containing a compound selected from the group consisting of, fatty compounds such as mineral oil, animal oil, oil vegetable, synthetic oil and silicon oil, and also alcohol, fatty acids and waxes, organic solvents, active agents of surface, ionic and non-ionic solubilizers and emulsifiers, thickening and gelling hydrophilic agents, such as carboxyvinyl polymers (for example, Carbomer), acrylic copolymers (for example, acrylates and alkylacrylates), polyacrylamides, polysaccharides, natural gums (e.g. gum xanthan); lipophilic thickening and gelling agents, such as modified clays (eg, bentonite), acid salts fatty metal, hydrophobic silica and polyethylene, perfumes and essential oils; astringent; antiperspirants; fluorides; humectants; sweeteners; softeners, excipients, antioxidants, sequestering agents, opacifiers, filters, compounds dyes, and pigments; and hydrophilic active ingredients or lipophilic. 6. Cosmetics and / or dermatological compositions comprising the antimicrobial system defined in any of claims 1 to 5. 7. Cosmetic composition for the skin or the oral care comprising the antimicrobial system defined in any of claims 1 to 5. 8. Composition according to claim 6 or 7 formed as an aqueous solution, solution hydro-alcoholic emulsion hydro-glycolic, micro-emulsion, aqueous or gel anhydride from a dispersion of the vesicles. 9. The use of the antimicrobial system is defined in any of claims 1 to 5 for the preparation of A composition for oral care. 10. The use of the antimicrobial system is defined in any one of claims 1 to 5 in a cosmetic and / or dermatological compositions against the microorganism. 11. The use of the antimicrobial system is defined in any one of claims 1 to 5 as a cosmetic and / or dermatological composition to avoid body odor.